Recent Advances in the Research and Development of Kinase-inhibitory Anticancer Molecules

Cancer is characterized by uncontrolled cell growth and proliferation following genetic mutation. It represents one of the most serious health issues worldwide and is the second leading cause of death. Therefore, it represents one of the greatest challenges to medical researchers, especially with the continued failure of current therapies from one side and the development of drug resistance from the other side. Kinase inhibition is one of the hotspot avenues for cancer treatment. Several kinase inhibitors are currently in clinical use for management of cancer, and many others are in clinical trials. Kinase inhibitors can also treat diseases other than cancer, including inflammatory and neurodegenerative disorders. Preferential kinase inhibitors that are relatively safe anticancer candidates are still needed to be developed to meet the unmet areas of disease therapy.

In cancer therapy, a challenging approach is to identify a biological target in cancer cells that abnormally potentiate their survival and to determine if it could be selectively targeted. Even better: this biological target is absent in the healthy cells and consequently they remain unaffected by a chemotherapeutic. Almost all the available anticancer agents lack this advantage. In this special issue, we welcome manuscripts that include the design of new candidates with an expected anticancer activity. The design of these compounds should be based on an acceptable rationale to ensure potency and selectivity against a limited number or a family of kinases. Protein kinases represent one of the most important molecular targets for cancer treatment. The rationale design can be either structure-based or in silico- based drug design or both.

We welcome Original Research, Review, Mini Review and Perspective articles on themes including, but not limited to:
• Design and synthesis of kinase inhibitors accompanied with their SAR and mechanistic study.
• Chemical structure-biological activity relationship, investigate the expected interaction with specific kinases, and correlate structures with their mode of action.
• Predicted biological interactions between new drug candidates and the claimed targets.
• Lead optimization to maximize the potency and selectivity against the target kinase(s).
• In vitro and in vivo biological evaluation of the target molecules.
• Studying the binding interactions either by X-ray crystallography or by computational studies.